Synthesis of novel benzo‐substituted macrocyclic schiff bases containing two triazole rings

A synthesis of a series of novel macrocyclic Schiff bases containing two triazole rings 10a,b, 11a,b, 34‐37 in good yields by heating the appropriate bis‐amines 1f, 6a,b, 31 with the corresponding bis‐aldehydes 2, 9a,b, 29 in refluxing acetic acid under high dilution conditions was described. Attempts to synthesize macrocyclic Schiff bases containing pyridine and two triazole rings were also described.     

Facile one-pot synthesis of 6-monosubstituted and 6,12-disubstituted 5,11-dihydroindolo[3,2-b]carbazoles and preparation of various functionalized derivatives

A facile three-stage, one-pot approach for the synthesis of a variety of novel 6-monosubstituted and 6,12-disubstituted 5,11-dihydroindolo[3,2-b]carbazoles, in moderate to good yields (20-50%), has been developed, based on the condensation of an indole and an aldehyde with a catalytic amount of iodine, followed by an acid-catalyzed intramolecular cyclization with an ortho ester. The parent indolo[3,2-b]carbazoles (ICZs) could be converted to various functional derivatives. Both N-alkylation and N-arylation were successfully accomplished, and azo-coupling, formylation, as well as bromination were performed in a regioselective way leading to the formation of novel functional 6,12-disubstituted indolo[3,2-b]carbazoles. Starting from a monoformylated indolocarbazole, novel benzimidazolyl-substituted derivatives were synthesized, while Suzuki cross-couplings on a monobrominated building block afforded a novel pathway toward functionally arylated ICZs.     

Preparation of superhydrophobic silicon oxide nanowire surfaces

The paper reports on the preparation of superhydrophobic amorphous silicon oxide nanowires (a-SiONWs) on silicon substrates with a contact angle greater than 150 degrees by means of surface roughness and self-assembly. Nanowires with an average mean diameter in the range 20-150 nm and 15-20 microm in length were obtained by the so-called solid-liquid-solid (SLS) technique. The porous nature and the high roughness of the resulting surfaces were confirmed by AFM imaging. The superhydrophobicity resulted from the combined effects of surface roughness and chemical modification with fluorodecyl trichlorosilane.     

Self-assembly of high-quality covalently bound organic monolayers onto silicon

A very mild method has been developed to obtain covalently attached alkyl monolayers from the attachment of 1-alkynes onto hydrogen-terminated silicon surfaces at room temperature in the dark. Apart from being the mildest method reported so far for the preparation of such monolayers, their quality, as indicated by water contact angles, XPS, and infrared spectroscopy, equals within experimental error that of the best reported alkyl monolayers on silicon.     

A generalization of the prolate spheroidal wave functions

Many systems of orthogonal polynomials and functions are bases of a variety of function spaces, such as the Hermite and Laguerre functions which are orthogonal bases of and and the Jacobi polynomials which are an orthogonal basis of a weighted The associated Legendre functions, and more generally, the spheroidal wave functions are also an orthogonal basis of

The prolate spheroidal wave functions, which are a special case of the spheroidal wave functions, possess a very surprising and unique property. They are an orthogonal basis of both and a subspace of known as the Paley-Wiener space of bandlimited functions. They also satisfy a discrete orthogonality relation. No other system of classical orthogonal functions is known to possess this strange property. This raises the question of whether there are other systems possessing this property.

The aim of the article is to answer this question in the affirmative by providing an algorithm to generate such systems and then demonstrating the algorithm by a new example.

     

Sage,Salvia officinalis L., Constituents,Hepatoprotective Activity,and Cytotoxicity Evaluations of the Essential Oils Obtained from Fresh and Differently Timed Dried Herbs: A Comparative Analysis

Sage, Salvia officinalis L., is used worldwide as an aromatic herb for culinary purposes as well as a traditional medicinal agent for various ailments. Current investigations exhibited the effects of extended dryings of the herb on the yields, composition, oil quality, and hepatoprotective as well as anti-cancer biological activities of the hydrodistillation-obtained essential oils from the aerial parts of the plant. The essential oils’ yields, compositions, and biological activities levels of the fresh and differently timed and room-temperature dried herbs differed significantly. The lowest yields of the essential oil were obtained from the fresh herbs (FH, 631 mg, 0.16%), while the highest yield was obtained from the two-week dried herbs (2WDH, 1102 mg, 0.28%). A notable decrease in monoterpenes, with increment in the sesquiterpene constituents, was observed for the FH-based essential oil as compared to all the other batches of the essential oils obtained from the different-timed dried herbs. Additionally, characteristic chemotypic constituents of sage, i.e., α-pinene, camphene, β-pinene, myrcene, 1, 8-cineole, α-thujone, and camphor, were present in significantly higher proportions in all the dried herbs’ essential oils as compared to the FH-based essential oil. The in vivo hepatoprotective activity demonstrated significant reductions in the levels of AST, ALT, and ALP, as well as a significant increase in the total protein (p < 0.05) contents level, as compared to the acetaminophen (AAP) administered experimental group of rats. A significant reduction (p < 0.05) in the ALT level was demonstrated by the 4WDH-based essential oil in comparison to the FH-based essential oil. The levels of creatinine, cholesterol, and triglycerides were reduced (p < 0.05) in the pre-treated rats by the essential oil batches, with non-significant differences found among them as a result of the herbs dryings based oils. A notable increase in the viability of the cells, and total antioxidant capacity (TAOxC) levels, together with the reduction in malondialdehyde (MDA) levels were observed by the essential oils obtained from all the batches as compared with the AAP-treated cell-lines, HepG-2, HeLa, and MCF-7, that indicated the in vitro hepatoprotective effects of the sage essential oils. However, significant improvements in the in vivo and in vitro hepatoprotective activities with the 4WDH-based oil, as compared to all other essential oil-batches and silymarin standard demonstrated the beneficial effects of the drying protocol for the herb for its medicinal purposes.     

Discovery,Development, and Patent Trends on Molnupiravir: A Prospective Oral Treatment for COVID-19

The COVID-19 pandemic needs no introduction at present. Only a few treatments are available for this disease, including remdesivir and favipiravir. Accordingly, the pharmaceutical industry is striving to develop new treatments for COVID-19. Molnupiravir, an orally active RdRp inhibitor, is in a phase 3 clinical trial against COVID-19. The objective of this review article is to enlighten the researchers working on COVID-19 about the discovery, recent developments, and patents related to molnupiravir. Molnupiravir was originally developed for the treatment of influenza at Emory University, USA. However, this drug has also demonstrated activity against a variety of viruses, including SARS-CoV-2. Now it is being jointly developed by Emory University, Ridgeback Biotherapeutics, and Merck to treat COVID-19. The published clinical data indicate a good safety profile, tolerability, and oral bioavailability of molnupiravir in humans. The patient-compliant oral dosage form of molnupiravir may hit the market in the first or second quarter of 2022. The patent data of molnupiravir revealed its granted compound patent and process-related patent applications. We also anticipate patent filing related to oral dosage forms, inhalers, and a combination of molnupiravir with marketed drugs like remdesivir, favipiravir, and baricitinib. The current pandemic demands a patient compliant, safe, tolerable, and orally effective COVID-19 treatment. The authors believe that molnupiravir meets these requirements and is a breakthrough COVID-19 treatment.     

Determination of trace impurities in nickel-based alloy using neutron activation analysis

A radiochemical neutron activation analysis procedure has been applied to investigate 40 major, minor, and trace impurities in nickel-based alloy. The extensive use of these alloys in the electronic industry, telecommunications, manufacturing of aircraft engine turbine blades and chemical equipments desires for their precise characterization. The concentration of nickel in the nickel-based alloy was found to be 56.8%, whereas Fe, Cr, Ca, Mg, Ce, Mn, Na and V were the major components of the alloy, which constituted to more than 26%. The rest of the elements was present in minor or trace levels. Most of the rare earth elements except Ce were also present in trace amounts. Neutron activation analysis technique was preferably used because of its good sensitivity and multielement determination capabilities for the characterization of high purity materials. The comparison of RNAA and INAA indicated improvement in the detection limits utilizing radiochemical separation procedures developed in the present work.